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Synthesis of some novel orsellinates and lecanoric acid related depsides as α-glucosidase inhibitors

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journal contribution
posted on 2018-07-03, 10:52 authored by Boddu Rama Krishna, Sistla Ramakrishna, Sangaraju Rajendra, Kuncha Madhusudana, Uppuluri Venkata Mallavadhani

Sixteen novel orsellinic esters (6a-l, 7a-d) along with four lecanoric acid related depsides (3a-c, 4) were synthesized and confirmed their structures by spectroscopic data (1H, 13C & HRMS). The synthesized compounds were evaluated for their in vitro α-glucosidase (Saccharomyces cerevisiae) inhibitory potential. Among the tested compounds, 3c (IC50: 140.9 μM) and 6c (IC50: 203.9 μM) displayed potent α-glucosidase inhibitory activity and found more active than the standard drug acarbose (IC50: 686.6 μM). Both the test compounds were subjected to in vivo antihyperglycemic activity using sucrose loaded model in Wistar rats and found compound 3c exhibited significant reduction in glucose levels.

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